Advances in covalent drug discovery

Nature Reviews Drug Discovery, Год журнала: 2022, Номер 21(12), С. 881 - 898

Опубликована: Авг. 25, 2022

Язык: Английский

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Recent progress in self-healing polymers and hydrogels based on reversible dynamic B–O bonds: boronic/boronate esters, borax, and benzoxaborole

Journal of Materials Chemistry A, Год журнала: 2021, Номер 9(26), С. 14630 - 14655

Опубликована: Янв. 1, 2021

Reversible boronic ester-based polymers/hydrogels achieve cutting-edge biomedical applications including drug delivery, adhesion, bioimplants, healthcare monitoring by self-healing, injectability, biocompatibility, multi-responsiveness to stimuli.

Язык: Английский

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Fighting antibiotic resistance—strategies and (pre)clinical developments to find new antibacterials

EMBO Reports, Год журнала: 2022, Номер 24(1)

Опубликована: Дек. 19, 2022

Язык: Английский

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The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

Chemical Reviews, Год журнала: 2024, Номер 124(5), С. 2441 - 2511

Опубликована: Фев. 21, 2024

Boron-containing compounds (BCC) have emerged as important pharmacophores. To date, five BCC drugs (including boronic acids and boroles) been approved by the FDA for treatment of cancer, infections, atopic dermatitis, while some natural are included in dietary supplements. Boron's Lewis acidity facilitates a mechanism action via formation reversible covalent bonds within active site target proteins. Boron has also employed development fluorophores, such BODIPY imaging, carboranes that potential neutron capture therapy agents well novel diagnostics therapy. The utility synthetic become multifaceted, breadth their applications continues to expand. This review covers many uses targets boron medicinal chemistry.

Язык: Английский

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The Boron Advantage: The Evolution and Diversification of Boron’s Applications in Medicinal Chemistry

Pharmaceuticals, Год журнала: 2022, Номер 15(3), С. 264 - 264

Опубликована: Фев. 22, 2022

In this review, the history of boron's early use in drugs, and boron functional groups medicinal chemistry applications are discussed. This includes diazaborines, boronic acids, benzoxaboroles, clusters, carboranes. Furthermore, critical developments from these highlighted along with recent developments, which exemplify potential prospects. Lastly, application form a prodrug, softdrug, as nanocarrier discussed to showcase emergence into new exciting fields. Overall, we emphasize evolution organoboron therapeutic agents privileged structures outline impact that has had on drug discovery development.

Язык: Английский

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An update on the discovery and development of reversible covalent inhibitors

Medicinal Chemistry Research, Год журнала: 2023, Номер 32(6), С. 1039 - 1062

Опубликована: Апрель 29, 2023

Язык: Английский

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Emerging Building Blocks for Medicinal Chemistry: Recent Synthetic Advances

European Journal of Organic Chemistry, Год журнала: 2021, Номер 2021(47), С. 6478 - 6510

Опубликована: Сен. 8, 2021

Abstract Current medicinal chemistry relies heavily on the quality of building blocks, i. e. reagents used to introduce chemical diversity into target molecules. The last decade witnessed an emergence many novel (or well‐overlooked old) chemotypes for drug discovery, which is related adapting new synthetic methodologies, designing sp 3 ‐enriched bioisosteres, paying attention previously underrated even unwanted) structural motifs, or combination thereof. In this review with 532 references, a survey selected that emerged recently in provided, focus synthesis corresponding blocks. Thus, saturated (hetero)aliphatic boronates, sulfonyl fluorides, sulfinates, non‐classical benzene isosteres, bicyclic morpholine/piperidine/piperazine analogs, as well gem ‐difluorinated cycloalkanes (as example emerging fluorinated motifs) are discussed.

Язык: Английский

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FDA-Approved Drugs for Hematological Malignancies—The Last Decade Review

Cancers, Год журнала: 2021, Номер 14(1), С. 87 - 87

Опубликована: Дек. 24, 2021

Hematological malignancies, also referred to as blood cancers, are a group of diseases involving abnormal cell growth and persisting in the blood, lymph nodes, or bone marrow. The development new targeted therapies including small molecule inhibitors, monoclonal antibodies, bispecific T engagers, antibody-drug conjugates, recombinant immunotoxins, and, finally, Chimeric Antigen Receptor (CAR-T) cells has improved clinical outcomes for cancers. In this review, we summarized 52 drugs that were divided into macromolecule agents, approved by Food Drug Administration (FDA) period between 2011 2021 treatment hematological malignancies. Forty them have been European Medicines Agency (EMA). We analyzed FDA-approved investigating both their structures mechanisms action. It should be emphasized number was significantly higher (46 drugs) than chemotherapy agents (6 drugs). highlight recent advances design used treat which make more effective less toxic.

Язык: Английский

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Saturated Boronic Acids, Boronates, and Trifluoroborates: An Update on Their Synthetic and Medicinal Chemistry

Chemistry - A European Journal, Год журнала: 2021, Номер 27(62), С. 15277 - 15326

Опубликована: Сен. 9, 2021

Abstract This review discusses recent advances in the chemistry of saturated boronic acids, boronates, and trifluoroborates. Applications title compounds design boron‐containing drugs are surveyed, with special emphasis on α‐amino derivatives. A general overview as modern tools to construct C(sp 3 )−C )‐heteroatom bonds is given, including developments Suzuki‐Miyaura Chan‐Lam cross‐couplings, single‐electron‐transfer processes metallo‐ organocatalytic photoredox reactions, transformations boron “ate” complexes. Finally, an attempt summarize current state art synthesis trifluoroborates made, a brief mention “classical” methods (transmetallation organolithium/magnesium reagents species, anti‐Markovnikov hydroboration alkenes, modification alkenyl compounds) focus methodologies (boronation alkyl (pseudo)halides, derivatives carboxylic alcohols, primary amines, boronative C−H activation, novel approaches alkene hydroboration, 1,2‐metallate‐type rearrangements).

Язык: Английский

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Electrochemical borylation of carboxylic acids

Proceedings of the National Academy of Sciences, Год журнала: 2021, Номер 118(34)

Опубликована: Авг. 17, 2021

Significance Boronic acids are one of the most useful functional groups in organic chemistry and can be used as intermediates synthesis or key motifs medicines. This work describes an extremely simple economical way to use electrochemistry convert carboxylic acids, through intermediacy redox-active esters, boronic acids. The scope this reaction is broad, mechanism has been thoroughly studied, it easily scaled up. Finally, application a complex polycyclopropane natural product demonstrated.

Язык: Английский

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